Ritschel W A, Shapiro-Jacobson M, Akileswaran R, Wetzelsberger K, Lücker P W
Division of Pharmaceutics and Drug Delivery Systems, University of Cincinnati Medical Center, Ohio, USA.
Methods Find Exp Clin Pharmacol. 1995 Sep;17(7):477-81.
Many drugs are bound to plasma proteins (PR) and/or to erythrocytes (RBC). The RBC count may change due to physiologic factors such as exposure to high altitude, or pathologic conditions such as anemia or as consequence of cancer treatment. The purpose of the investigation was to study the influence of 1) drug concentration, and 2) number of RBC on erythrocyte uptake or binding using meperidine as a model drug (M). Human RBC concentrated blood was used and blood chemistry determined. Using human plasma (P) dilutions were made containing 9.9, 7.62, 5.87 and 4.11 million RBC mm3. The whole blood (WB) samples were spiked with M to result in 10, 25, 50, or 75 micrograms/ml. Increasing concentrations of M within each group of same RBC count did not influence percentage of erythrocyte uptake/binding. Increase in RBC count from 4.11 to 9.9 million/mm3 resulted in significant increase in erythrocyte uptake from 77.1% to 94.7% and increase in PR binding from 37.2% to 87.4%.
许多药物会与血浆蛋白（PR）和/或红细胞（RBC）结合。红细胞计数可能会因生理因素（如暴露于高海拔地区）或病理状况（如贫血或癌症治疗的结果）而发生变化。本研究的目的是使用哌替啶作为模型药物（M），研究1）药物浓度和2）红细胞数量对红细胞摄取或结合的影响。使用了人红细胞浓缩血液并测定了血液化学成分。使用人血浆（P）进行稀释，制成每立方毫米含有990万、762万、587万和411万个红细胞的溶液。全血（WB）样本中加入M，使其浓度达到10、25、50或75微克/毫升。在相同红细胞计数的每组中，M浓度的增加并未影响红细胞摄取/结合的百分比。红细胞计数从每立方毫米411万个增加到990万个，导致红细胞摄取从77.1%显著增加到94.7%，血浆蛋白结合从37.2%增加到87.4%。
